Bv8/PK2 and prokineticin receptors: a druggable pronociceptive system

Curr Opin Pharmacol. 2012 Feb;12(1):62-6. doi: 10.1016/j.coph.2011.10.023. Epub 2011 Nov 30.

Abstract

Mammalian Bv8 (also called prokineticin 2) is a secreted protein that regulates diverse biological processes including pain perception. It belongs to a new family of chemokines, which activate two G-protein linked receptors (prokineticin receptor 1 and 2, PKR1 and PKR2) expressed in regions of the nervous system associated with pain and in cells participating to immuno-inflammatory responses. Primary sensitive neurons co-express PKRs and the transient potential receptor vanilloid 1, cooperating in nociceptor sensitization. Bv8, strongly upregulated in neutrophils and other inflammatory cells, is a main pronociceptive mediator in inflamed tissues, where it sensitizes peripheral nociceptors, stimulates neutrophil chemotaxis and modulates the release of inflammatory and pronociceptive cytokines. Availability of a nonpeptide PKR antagonist, leading to blockade of the Bv8/PKR system, ameliorates pain arising from tissue injury and reduces the time required for recovery from injury.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Analgesics / pharmacology*
  • Animals
  • Gastrointestinal Hormones / metabolism*
  • Humans
  • Neuropeptides / metabolism*
  • Pain / drug therapy*
  • Pain / metabolism
  • Receptors, G-Protein-Coupled / metabolism*
  • Receptors, Peptide / metabolism*

Substances

  • Analgesics
  • Gastrointestinal Hormones
  • Neuropeptides
  • PROK2 protein, human
  • Prok2 protein, mouse
  • Receptors, G-Protein-Coupled
  • Receptors, Peptide